期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 28, 期 9, 页码 1540-1544出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.03.069
关键词
Malaria; Falcipain-2 Peptidomimetic-nitrile; 3-Pyridine; Selective
资金
- CNCCS scarl
- POR FESR Programme (POR FESR) Insieme per Vincere, under the Project AICI - Small Molecules con attivita antiparassitaria
Falcipain-2 (FP2) is an essential enzyme in the lifecycle of malaria parasites such as Plasmodium falciparum, and its inhibition is viewed as an attractive mechanism of action for new anti-malarial agents. Selective inhibition of FP2 with respect to a family of human cysteine proteases (that include cathepsins B, K, L and S) is likely to be required for the development of agents targeting FP2. Here we describe a series of P2-modified aminonitrile based inhibitors of FP2 that provide a clear strategy toward addressing selectivity for the P. falciparum and show that it can provide potent FP2 inhibitors with strong selectivity against all four of these human cathepsin isoforms. (C) 2018 Elsevier Ltd. All rights reserved.
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